LG101506
Based on 1 Customer Validation
LG101506 is a selective and orally active RXR modulator with a Ki of 2.7 nM for RXRα. LG101506 can be used for the research of type 2 diabetes and cancer.
For research use only. We do not sell to patients.
- Purity : 98.41%
- CAS No.: 331248-11-4
- Formula: C25H34F2O3
- Molecular Weight:420.53
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
Ki: 2.7 nM (RXRα)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
11 nM
Compound: LG0101506
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Transcriptional activation in CV-1 cells expressing Retinoic X receptor alpha
Transcriptional activation in CV-1 cells expressing Retinoic X receptor alpha
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[PMID: 15006411] |
| CV-1 | EC50 |
131.5 nM
Compound: 4
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In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined
In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined
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[PMID: 12954061] |
| CV-1 | EC50 |
3.1 nM
Compound: 1
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Synergistic activation of BRL-49653 mediated PPAR gamma and retinoid X receptor alpha expressed in CV-1 cell transcriptional activation assay
Synergistic activation of BRL-49653 mediated PPAR gamma and retinoid X receptor alpha expressed in CV-1 cell transcriptional activation assay
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[PMID: 12951091] |
| CV-1 | IC50 |
8 nM
Compound: 4
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In vitro transcriptional activation in CV-1 cells expressing RXR-alpha
In vitro transcriptional activation in CV-1 cells expressing RXR-alpha
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[PMID: 12954061] |
In Vitro
LG101506 synergizes with BRL 49653 (HY-17386) to enhance activation at the RXR/PPARγ heterodimer with an EC50 of 3.1 nM[1].
LG101506 (15.6-1000 nM) blocks the production of NO in a dose-dependent manner in RAW264.7 stimulated with LPS (HY-D1056) for 24 hours[2].
LG101506 (100-1000 nM; 24 h) inhibits inflammatory pathways induced by LPS (HY-D1056) or TNFα in RAW264.7 cells[2].
LG101506 (30 and 100 nM; 1-24 h) induces differentiation in U937 leukemia cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 cells
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Concentration:100, 300 and 1000 nM
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Incubation Time:24 h
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Result:Markedly reduced protein levels of COX-2. Pretreatment prevented the degradation of IκBα in RAW cells stimulated with TNFα. Enhanced Erk phosphorylation, which peaked at 8 hours.
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Cell Line:U937 leukemia cells
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Concentration:30 and 100 nM
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Incubation Time:1, 2, 8 and 24 h
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Result:Enhanced phosphorylation of Akt in U937 cells within 1 hour, which increased further at 8 hours.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A/J mice, lung carcinogenesis model[2]
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Dosage:40 mg/kg diet or approximately 10 mg/kg body weight
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Administration:Oral, for 16 weeks
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Result:Reduced the number of lung tumors, the average tumor burden, the size and histopathology of lung tumors.
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Animal Model:Male ICR mice[1]
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Dosage:30 mg/kg
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Administration:Oral (Pharmacokinetic Analysis)
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Result:In vivo evaluation of oral exposure of LG101506[1]
Compd Dose (mg/kg) Oral AUC(0-6 h) (μg•h/mL) Tmax (h) Cmax (μg•h/mL) LG101506 30 2.09±0.45 1 1.2±0.28
Data collected in male ICR mouse using a dose formulation of the free acid in CMC/SLS/Povidone (30 mg/kg). Timepoints: 1, 3, 8 h (serial sacrifice, n=3/time point).
Chemical Information
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CAS No. 331248-11-4
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Appearance Solid
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Molecular Weight 420.53
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Formula C25H34F2O3
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Color White to off-white
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SMILES
FC(F)COC1=C(C=C(C=C1/C(C)=C\C=C\C(C)=C\C(O)=O)C(C)(C)C)C(C)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 33.33 mg/mL (79.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.94 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Gernert DL, et al. Design and synthesis of fluorinated RXR modulators. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3191-5. [Content Brief]
[2]. Cao M, et al. The Rexinoids LG100268 and LG101506 Inhibit Inflammation and Suppress Lung Carcinogenesis in A/J Mice. Cancer Prev Res (Phila). 2016 Jan;9(1):105-14. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3780 mL | 11.8898 mL | 23.7795 mL | 59.4488 mL |
| 5 mM | 0.4756 mL | 2.3780 mL | 4.7559 mL | 11.8898 mL | |
| 10 mM | 0.2378 mL | 1.1890 mL | 2.3780 mL | 5.9449 mL | |
| 15 mM | 0.1585 mL | 0.7927 mL | 1.5853 mL | 3.9633 mL | |
| 20 mM | 0.1189 mL | 0.5945 mL | 1.1890 mL | 2.9724 mL | |
| 25 mM | 0.0951 mL | 0.4756 mL | 0.9512 mL | 2.3780 mL | |
| 30 mM | 0.0793 mL | 0.3963 mL | 0.7927 mL | 1.9816 mL | |
| 40 mM | 0.0594 mL | 0.2972 mL | 0.5945 mL | 1.4862 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1890 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3963 mL | 0.9908 mL |
LG101506 Related Classifications
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